G protein-coupled receptors (GPCRs) represent the largest and most diverse family of receptors in the human body, playing essential roles in neurotransmission, immune regulation, endocrine signaling, and metabolic homeostasis. Currently, more than 30% of approved drugs directly or indirectly target GPCRs. With the rapid advances in research on metabolic disorders, cancer immunotherapy, and neurological diseases, an increasing number of orphan GPCRs have been identified as being closely associated with disease pathogenesis, further reinforcing GPCRs as one of the most promising and enduring classes of drug discovery targets.

However, the unique structural characteristics of GPCRs pose significant challenges for both basic research and drug development. As highly hydrophobic, multi-pass transmembrane proteins, GPCRs rely on an intact lipid membrane environment to maintain their native conformations. Once removed from the cell membrane, they are prone to conformational changes or even loss of function. Consequently, traditional detection methods based on denatured or fixed conditions—such as Western blotting, ELISA, or immunohistochemistry—often fail to accurately reflect GPCR expression on the surface of living cells or their physiological relevance. This limitation significantly hinders reliable receptor characterization, signaling mechanism studies, and the accurate screening of drug candidates.

To truly understand GPCR biology and advance drug development, it is essential to directly detect and quantify cell-surface receptors in their native conformation on living cells. By enabling analysis in an intact membrane environment, GPCR flow cytometry antibodies have become a critical tool for evaluating receptor expression, antibody binding, and target accessibility.

Addressing the conformational dependence of GPCRs and the need for live-cell analysis, flow cytometry antibodies deliver the following core values in research and drug discovery:

3. Applications of GPCR Flow Cytometry Antibodies

Leveraging the ability to directly detect GPCRs on living cells by flow cytometry, GPCR flow cytometry antibodies demonstrate significant advantages in both research and development. By preserving native conformation recognition, enabling quantitative single-cell analysis, integrating seamlessly with multiple functional assays, and supporting diverse cell types, these antibodies provide a more physiologically relevant approach for GPCR expression validation, antibody screening, and functional studies.

The figure below summarizes the key advantages of GPCR flow cytometry antibodies across major application scenarios.

Preservation of Native Conformation Recognition

Antibodies recognize receptors in their native state on the surface of living cells, without relying on denaturation or fixation, thereby more accurately reflecting physiological conditions.

Compatibility with Functional Assays

Can be combined with Ca²⁺ flux assays, signaling pathway analyses, and internalization studies to establish a comprehensive GPCR research workflow.

Quantitative Analysis of Expression Levels

Flow cytometry enables precise quantification at single-cell resolution, facilitating direct comparison of GPCR expression levels across different treatment conditions.

Applicable to Multiple Cell Types

Suitable for rapid assessment of receptor distribution in primary cells, transfected cell lines, and heterogeneous immune cell populations.

GPCRs are complex seven-transmembrane proteins whose native conformations are difficult to preserve with traditional antibodies, which often require permeabilization and can disrupt membranes, cause signal loss, or introduce false positives. DIMA’s GPCR flow cytometry antibodies overcome these limitations by using native-conformation antigens generated through our DiMPro^TM Nanodisc platform. These antibodies specifically recognize GPCR epitopes on the surface of live cells, enabling direct detection without permeabilization. This approach allows researchers to measure GPCR expression and conformational changes under conditions that closely reflect physiological states, providing more reliable, accurate, and biologically meaningful data for GPCR research and drug development.

Key advantages:

DIMA offers an extensive library of GPCR flow cytometry antibodies, covering multiple research areas including immunology, neuroscience, metabolism, and oncology:

Case Studies

Our GPCR antibodies are carefully developed and validated to target native extracellular epitopes, ensuring high specificity in live-cell flow assays.

Anti-CCR1 antibody(DMC465); IgG1 Chimeric mAb

(A) DMC100465 does not bind to CHO-S cells that do not express CCR1.
(B) A clear peak shift of DMC100465 was seen compared to the control when incubated with CCR1-expressing 8226 cells, indicating strong binding of DMC100465 to CCR1. Antibodies were incubated at 5 μg/ml.

Anti-CCR6 antibody(DMC477); IgG1 Chimeric mAb

(A) DMC100477 does not bind to CHO-S cells that do not express CCR6.
(B) A clear peak shift of DMC100477 was seen compared to the control when incubated with CCR6-expressing Huh7 cells, indicating strong binding of DMC100477 to CCR6. Antibodies were incubated at 5 μg/mL.

Anti-GPRC5D antibody(DM91); Rabbit mAb

(A) DME100091 does not bind to Jurkat cells that do not express GPRC5D.

(B) A clear peak shift of DME100091 was seen compared to the control when incubated with GPRC5D-expressing MM.1S cells, indicating strong binding of DME100091 to GPRC5D. Antibodies were incubated at 5 µg/mL.